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Outcome of children with traumatic brain injury in rural Malaysia

Kumaraswamy N, Naziah A, Abdullah J, Ariff MMed AR, Abdullah MR, Ghazaime G

J Clin Neurosci, 2002 May;9(3):251-5.
PMID: 12093129

Malaysia had the second highest crude accident rate in the world until 1998. Most children who were involved in these road traffic accidents required intensive neurosurgical care management. We report a prospective study on 36 paediatric neurotrauma patients in rural North East West Malaysia who underwent uniform intensive therapy and were subsequently followed up over a period of 2 years. The modified paediatric Glasgow Coma Scale with support of the revised Wechlser Intelligence Scale for children was used to test the outcome of these children over a period of two years. All patients were managed aggressively in our intensive care as well as our high dependency units. Our results indicate that improvement in outcome is seen after a six month period. Midline shift, duration of coma and duration of transport were found to be significant variables associated with bad outcome. Other variables i.e. age, sex, Glasgow Coma Scale on admission and on site, and lesions of the dominant lobe were not found to be associated with good outcome in these patients.
Fulltext Breast cancer in pregnancy--our experience with six patients in the University Hospital, Kuala Lumpur

Yip CH, Taib NA, Abdullah MM, Wahid I

Med J Malaysia, 2000 Sep;55(3):308-10.
PMID: 11200709

Presentation of breast cancer during pregnancy is a rare situation and one that requires a multidisciplinary approach involving an obstetrician, surgeon and oncologist. Management should be along the same principles as in non-pregnant patients and delay is not justifiable. Mastectomy and axillary clearance is the best option, followed by chemotherapy, which is safe after the first trimester. Radiation if required should be delayed until after delivery of the baby. We present here our experience with 6 patients who presented with breast cancer during pregnancy. Five patients refused any treatment until after delivery, while one underwent only a mastectomy and axillary clearance. The outcome was poor; all of them died between 14 months and 52 months. The poor outcome probably reflects the late stage at presentation in four of the patients (State 3 and 4) rather than the delay in treatment, while delay in treatment in the two who presented with early cancer (Stage 1 and 2) led to a more advanced stage after delivery.
Does ascariasis, trichuriasis and hookworm infection predispose to non-specific abdominal symptoms among adults in endemic areas?

Raj SM, Anteson R, Sivakumaran S, Abdullah MR, Low HC

Trop Doct, 1994 Apr;24(2):88-9.
PMID: 8009635
Do ascariasis, trichuriasis and hookworm infections predispose to non-specific abdominal symptoms among adults in endemic areas?

Raj SM, Anteson R, Sivakumaran S, Abdullah MR, Low HC

Trop Doct, 1993 Oct;23(4):166-7.
PMID: 8273160
Fulltext HLA-DRB1*04 as a Risk Allele to Systemic Lupus Erythematosus and Lupus Nephritis in the Malay Population of Malaysia

Selvaraja M, Chin VK, Abdullah M, Arip M, Amin-Nordin S

Front Med (Lausanne), 2020;7:598665.
PMID: 33644084 DOI: 10.3389/fmed.2020.598665

Systemic lupus erythematosus (SLE) is a chronic autoimmune disease afflicting multiple organs. Lupus nephritis (LN) is a serious complication of SLE and remains a major cause of mortality and morbidity. Curative therapy remains unavailable as etiology from genetic and environmental factors is still unclear. The present study was conducted to elucidate the link between HLA-DRB1 gene polymorphisms with SLE and LN through clinical and laboratory/biological presentations in a population of Malaysian Malay females with SLE. A total of 100 Malay female SLE patients inclusive of 70 SLE patients without LN and 30 patients with LN were included in this study. HLA-DRB1 allele examination in SLE patients was performed using PCR-SSO, and the alleles' frequencies were compared with 951 publicly available datasets representing Malay healthy controls in Malaysia. Cytokines and free radical levels were detected by ELISA and bead-based multiplexed Luminex assays. The association between HLA-DRB1 alleles with clinical and serological manifestations and immune mediators was analyzed using different statistical approaches whenever applicable. Our study showed that HLA-DRB1*0405, HLA-DRB1*1502, and HLA-DRB1*1602 were associated with the increased risk of SLE while HLA-DRB1*1201 and HLADRB1*1202 alleles were associated with a lower risk of SLE development. Furthermore, HLA-DRB1*04 showed significant association to LN and arthritis while HLA-DRB1*15 was significantly associated with oral ulcer in Malay SLE patients. Association analysis of HLA-DRB1*04 with clinical and biological factors revealed that HLA-DRB1*04 was significantly associated with Systemic Lupus Erythematosus Disease Activity Index (SLEDAI) scores, anti-nuclear antibody (ANA), C-reactive protein (CRP) in the blood, and total protein in the urine. SLE carriers with the HLA-DRB1*04 allele were significantly correlated to the increased levels of cytokines (IFN-y, GM-CSF, IL-17F, IL-18, IL-21, and VEGF) and were significantly showing negative correlation to IL-5 and free radicals (LPO and catalase enzyme) levels compared to SLE carriers without HLA-DRB1*04 allele. The results suggested that disease severity in SLE may be determined by HLA-DRB1 alleles. The risk of HLA-DRB1*04 allele with LN was supported by the demonstration of an intense inflammatory response in Malay SLE patients in Malaysia. More studies inclusive of a larger and multiple SLE cohorts in the future are warranted to validate these findings.
Fulltext The Roles of Non-Coding RNAs in Tumor-Associated Lymphangiogenesis

Md Yusof K, Rosli R, Abdullah M, A Avery-Kiejda K

Cancers (Basel), 2020 Nov 06;12(11).
PMID: 33172072 DOI: 10.3390/cancers12113290

Lymphatic vessels are regarded as the "forgotten" circulation. Despite this, growing evidence has shown significant roles for the lymphatic circulation in normal and pathological conditions in humans, including cancers. The dissemination of tumor cells to other organs is often mediated by lymphatic vessels that serve as a conduit and is often referred to as tumor-associated lymphangiogenesis. Some of the most well-studied lymphangiogenic factors that govern tumor lymphangiogenesis are the vascular endothelial growth factor (VEGF-C/D and VEGFR-2/3), neuroplilin-2 (NRP2), fibroblast growth factor (FGF), and hepatocyte growth factor (HGF), to name a few. However, recent findings have illustrated that non-coding RNAs are significantly involved in regulating gene expression in most biological processes, including lymphangiogenesis. In this review, we focus on the regulation of growth factors and non-coding RNAs (ncRNAs) in the lymphatic development in normal and cancer physiology. Then, we discuss the lymphangiogenic factors that necessitate tumor-associated lymphangiogenesis, with regards to ncRNAs in various types of cancer. Understanding the different roles of ncRNAs in regulating lymphatic vasculature in normal and cancer conditions may pave the way towards the development of ncRNA-based anti-lymphangiogenic therapy.
Hedgehog signalling molecule, SMO is a poor prognostic marker in bladder cancer

Mohd Ariffin K, Abd Ghani F, Hussin H, Md Said S, Yunus R, Veerakumarasivam A, et al.

Malays J Pathol, 2021 Apr;43(1):49-54.
PMID: 33903305

INTRODUCTION: Hedgehog (HH) pathway is an important signalling cascade for growth and patterning during embryonic development. Constitutive activation of Hedgehog pathway can be found in various types of malignancies including medulloblastoma, basal cell carcinoma, gastrointestinal, breast, pancreatic, prostate cancer and leukaemia. Little is known about the expression and role of Hedgehog signalling in bladder cancer.
MATERIALS AND METHODS: The purpose of this study was to investigate the immunohistochemical expression of SMO in 112 bladder cancer cases and determine their association with demographic and clinicopathological parameters. Bladder cancer tissues were obtained from the Hospital Kuala Lumpur.
RESULTS: SMO was expressed in the cytoplasm of all cases of bladder cancer. 6 cases (5.4%) showed low expression, while 106 cases (94.6%) showed high expression. Positive expression of SMO protein was correlated with a few variables which include grade and stage of tumour, lymph node metastasis and distant metastasis. SMO expression showed statistically significant association with higher grade (p=0.001) and higher stage (p=0.042) of bladder cancer. SMO expression also showed borderline association with lymph node metastasis (p=0.056).
CONCLUSION: These findings indicate that SMO expression may be a poor prognostic marker in bladder cancer.
Comparative proteomic analysis of oil palm (Elaeis guineensis Jacq.) during early fruit development

Kok SY, Namasivayam P, Ee GC, Ong-Abdullah M

J Proteomics, 2021 02 10;232:104052.
PMID: 33262095 DOI: 10.1016/j.jprot.2020.104052

To gain insights on protein changes in fruit setting and growth in oil palm, a comparative proteomic approach was undertaken to study proteome changes during its early development. The variations in the proteome at five early developmental stages were investigated via a gel-based proteomic technique. A total of 129 variant proteins were determined using mass spectrometric analysis, resulting in 80 identifications. The majority of the identified protein species were classified as energy and metabolism, stress response/defence and cell structure during early oil palm development representing potential candidates for the control of final fruit size and composition. Seven prominent protein species were then characterised using real-time polymerase chain reaction to validate the mRNA expression against the protein abundant profiles. Transcript and protein profiles were parallel across the developmental stages, but divergent expression was observed in one protein spot, indicative of possible post-transcriptional events. Our results revealed protein changes in early oil palm fruit development provide valuable information in the understanding of fruit growth and metabolism during early stages that may contribute towards improving agronomic traits. BIOLOGICAL SIGNIFICANCE: Two-dimensional gel electrophoresis coupled with mass spectrometry approach was used in this study to identify differentially expressed proteins during early oil palm fruit development. A total of 80 protein spots with significant change in abundance were successfully identified and selected genes were analysed using real time PCR to validate their expression. The dynamic changes in oil palm fruit proteome during early development were mostly active in primary and energy metabolism, stress responses, cell structure and protein metabolism. This study reveals the physiological processes during early oil palm fruit development and provides a reference proteome for further improvements in fruit quality traits.
Fulltext Increase in tumour-infiltrating lymphocytes with regulatory T cell immunophenotypes and reduced zeta-chain expression in nasopharyngeal carcinoma patients

Yip WK, Abdullah MA, Yusoff SM, Seow HF

Clin Exp Immunol, 2009 Mar;155(3):412-22.
PMID: 19220831 DOI: 10.1111/j.1365-2249.2008.03793.x

The pathological significance of the mechanisms of tumour immune-evasion and/or immunosuppression, such as loss of T cell signalling and increase in regulatory T cells (T(regs)), has not been well established in the nasopharyngeal carcinoma (NPC) microenvironment. To evaluate the T(reg) immunophenotypes in tumour-infiltrating lymphocytes (TILs), we performed a double-enzymatic immunostaining for detection of forkhead box P3 (FoxP3) and other markers including CD4, CD8, and CD25 on 64 NPC and 36 non-malignant nasopharyngeal (NP) paraffin-embedded tissues. Expression of CD3 zeta and CD3 epsilon was also determined. The prevalence of CD4(+)FoxP3(+) cells in CD4(+) T cells and the ratio of FoxP3(+)/CD8(+) were increased significantly in NPC compared with those in NP tissues (P < 0.001 and P = 0.025 respectively). Moreover, the ratio of FoxP3(+)/CD25(+)FoxP3(-) in NPC was significantly lower than that in NP tissues (P = 0.005), suggesting an imbalance favouring activated phenotype of T cells in NPC. A significant negative correlation between the abundance of FoxP3(+) and CD25(+)FoxP3(-) cells (P < 0.001) was also identified. When histological types of NPC were considered, a lower ratio of FoxP3(+)/CD25(+)FoxP3(-) was found in non-keratinizing and undifferentiated carcinomas. Increased CD4(+)FoxP3(+)/CD4(+) proportion and FoxP3(+)/CD8(+) ratio were associated with keratinizing squamous cell carcinoma. A reduced expression of CD3 zeta in TILs was found in 20.6% of the NPC tissues but none of the NP tissues. These data provide evidence for the imbalances of T(reg) and effector T cell phenotypes and down-regulation of signal-transducing molecules in TILs, supporting their role in suppression of immune response and immune evasion of NPC.
Development of Cell Penetrating Peptides for Effective Delivery of Recombinant Factors into Target Cells

Vijakumaran U, Nordin F, Hamid ZA, Abdullah M, Jun TG

Protein Pept Lett, 2020;27(11):1092-1101.
PMID: 32484079 DOI: 10.2174/0929866527666200525164135

The cell membrane is a protective layer that strictly controls the passage of molecules restricting the delivery of biomolecules such as drugs, oligonucleotides, peptides, and siRNA into the cells. This shortcoming has been overcome by the discovery of Cell-Penetrating Peptides (CPPs) that has undergone 30 years of evolution. To date, CPPs are largely modified to improve its efficacy and to suit the different delivery applications. The modes of CPPs penetration are still an unresolved mystery and requires further investigations to increase its effectiveness and to diversify its use. Despite having huge potential as a biomolecule carrier, CPPs also have some drawbacks. In this review, the natural and synthetic CPPs, the modifications that have been conducted on CPPs to improve its efficacy, its extended applications, modes of penetration and limitation as well as challenges will be discussed.
Fulltext Recent Updates on Mechanisms of Resistance to 5-Fluorouracil and Reversal Strategies in Colon Cancer Treatment

Azwar S, Seow HF, Abdullah M, Faisal Jabar M, Mohtarrudin N

Biology (Basel), 2021 Aug 31;10(9).
PMID: 34571731 DOI: 10.3390/biology10090854

5-Fluorouracil (5-FU) plus leucovorin (LV) remain as the mainstay standard adjuvant chemotherapy treatment for early stage colon cancer, and the preferred first-line option for metastatic colon cancer patients in combination with oxaliplatin in FOLFOX, or irinotecan in FOLFIRI regimens. Despite treatment success to a certain extent, the incidence of chemotherapy failure attributed to chemotherapy resistance is still reported in many patients. This resistance, which can be defined by tumor tolerance against chemotherapy, either intrinsic or acquired, is primarily driven by the dysregulation of various components in distinct pathways. In recent years, it has been established that the incidence of 5-FU resistance, akin to multidrug resistance, can be attributed to the alterations in drug transport, evasion of apoptosis, changes in the cell cycle and DNA-damage repair machinery, regulation of autophagy, epithelial-to-mesenchymal transition, cancer stem cell involvement, tumor microenvironment interactions, miRNA dysregulations, epigenetic alterations, as well as redox imbalances. Certain resistance mechanisms that are 5-FU-specific have also been ascertained to include the upregulation of thymidylate synthase, dihydropyrimidine dehydrogenase, methylenetetrahydrofolate reductase, and the downregulation of thymidine phosphorylase. Indeed, the successful modulation of these mechanisms have been the game plan of numerous studies that had employed small molecule inhibitors, plant-based small molecules, and non-coding RNA regulators to effectively reverse 5-FU resistance in colon cancer cells. It is hoped that these studies would provide fundamental knowledge to further our understanding prior developing novel drugs in the near future that would synergistically work with 5-FU to potentiate its antitumor effects and improve the patient's overall survival.
Pathology and Host Immune Evasion During Human Leptospirosis: a Review

Chin VK, Basir R, Nordin SA, Abdullah M, Sekawi Z

Int Microbiol, 2020 May;23(2):127-136.
PMID: 30875033 DOI: 10.1007/s10123-019-00067-3

Human leptospirosis is considered as one of the most widespread and potentially fatal zoonotic diseases that causes high mortality and morbidity in the endemic regions of tropical and subtropical countries. The infection can arise from direct or indirect exposure of human through contaminated environment that contains leptospires or animal reservoirs that carry leptospires. The clinical manifestations during human leptospirosis ranges from asymptomatic, mild infections to severe and life-threatening complications involving multi-organ failures with kidneys, lungs and liver severely affected. Despite much efforts have been put in to unravel the pathogenesis during human leptospirosis, it remains obscure to which extent the host factors or the pathogen itself contribute towards the pathogenesis. Host innate immunity, especially, polymorphonuclear neutrophils and complement system are involved in the first line of defense during human leptospirosis. However, pathogenic Leptospira has acquired diverse evasion strategies to evade from host immunity and establish infection in infected hosts. Hence, in this review, we focus on organs pathology during human leptospiral infection and host evasion strategies employed by Leptospira. A profound understanding on leptospiral immunity and how Leptospira subvert the immune system may provide new insights on the development of therapeutic regimens against this species in future.
Comparative pharmacokinetic study of oral and rectal formulations of artesunic acid in healthy volunteers

Navaratnam V, Mansor SM, Mordi MN, Akbar A, Abdullah MN

Eur J Clin Pharmacol, 1998 Jul;54(5):411-4.
PMID: 9754985

OBJECTIVE: A single cross-over, comparative pharmacokinetic study of oral and rectal formulations of 200 mg artesunic acid in 12 healthy Malaysian volunteers is reported.
METHODS: Plasma concentrations of artesunic acid and dihydroartemisinin were determined simultaneously by HPLC with electrochemical detection. The test drug was well tolerated and no undesirable adverse effects were observed.
RESULTS: Comparison of pharmacokinetic parameters of artesunic acid after oral and rectal administration showed statistically significant differences in t(max) and AUC, with no changes for Cmax and t1/2. As for dihydroartemisinin, differences were observed for t(max) and Cmax but not for AUC.
CONCLUSION: There appear to be pharmacokinetic differences between oral and rectal modes of administration. The significance of these findings should be explored in malaria patients before appropriate therapeutic regimens are devised.
Fulltext Nasopharyngeal carcinoma in Brunei Darussalam: low incidence among the Chinese and an evaluation of antibodies to Epstein-Barr virus antigens as biomarkers

Yeo CH, Hsien YC, Abdullah MS, Telesinghe PU, Ramasamy R

Singapore Med J, 2009 Apr;50(4):371-7.
PMID: 19421680

Little or no information is available on the prevalence of nasopharyngeal carcinoma (NPC) among different ethnic groups in Brunei, or how useful plasma IgA antibodies are against viral capsid antigen (VCA) and early antigen (EA) in the diagnosis of NPC, even though they are routinely measured in patients suspected to have NPC.
Fulltext Structural changes and band gap tunability with incorporation of n-butylammonium iodide in perovskite thin film

Rebecca LWX, Burhanudin ZA, Abdullah M, Saheed MSM

Heliyon, 2020 Feb;6(2):e03364.
PMID: 32072054 DOI: 10.1016/j.heliyon.2020.e03364

The current work presents structural change and band gap tunability using hybrid organic-inorganic perovskite with the incorporation of long chain ammonium halide. Thin films of MAPbI3 with different ratio of n-butylammonium iodide (BAI) have been successfully deposited on the substrate using a single step coating technique. X-ray diffraction scans revealed the transition of the 3D structure of MAPbI3 to quasi-2D perovskite structure when BAI loading increase with a crystallite size range approximately 16 nm. This structural changeis reflected in the band gap as it increased from 1.59 eV for bulk crystal MAPbI3 to 2.13 eV for BAI and MAPbI3 ratio of 1:1. Correspondingly, photoluminescence measurement showed a blue shift in perovskite emission due to the transition of 3D to 2D layered structure perovskite. Raman spectra confirm that all fabricated films are of pristine quality and no corresponding degradation peaks of PbI2 is observed. These characteristics are important to address the single step deposition method of hybrid perovskite for perovskite solar cells application.
Utilization of solar energy for wastewater treatment: Challenges and progressive research trends

Pandey AK, Reji Kumar R, B K, Laghari IA, Samykano M, Kothari R, et al.

J Environ Manage, 2021 Nov 01;297:113300.
PMID: 34293672 DOI: 10.1016/j.jenvman.2021.113300

This article offers a trend of inventions and implementations of photocatalysis process, desalination technologies and solar disinfection techniques adapted particularly for treatment of industrial and domestic wastewater. Photocatalysis treatment of wastewater using solar energy is a promising renewable solution to reduce stresses on global water crisis. Rendering to the United Nation Environment Programme, 1/3 of world population live in water-stressed countries, while by 2025 about 2/3 of world population will face water scarcity. Major pollutants exhibited from numerous sources are critically discussed with focus on potential environmental impacts & hazards. Treatment of wastewater by photocatalysis technique, solar thermal electrochemical process, solar desalination of brackish water and solar advanced oxidation process have been presented and systematically analysed with challenges. Both heterogenous and homogenous photocatalysis techniques employed for wastewater treatment are critically reviewed. For treating domestic wastewater, solar desalination technologies adopted for purifying brackish water into potable water is presented along with key challenges and remedies. Advanced oxidation process using solar energy for degradation of organic pollutant is an important technique to be reviewed due to their effectiveness in wastewater treatment process. Present article focused on three key issues i.e. major pollutants, wastewater treatment techniques and environmental benefits of using solar power for removal of pollutants. The review also provides close ideas on further research needs and major concerns. Drawbacks associated with conventional wastewater treatment options and direct solar energy-based wastewater treatment with energy storage systems to make it convenient during day and night both listed. Although, energy storage systems increase the overall cost of the wastewater treatment plant it also increases the overall efficiency of the system on environmental cost. Cost-efficient wastewater treatment methods using solar power would significantly ensure effective water source utilization, thereby contributing towards sustainable development goals.
Novel black yeast-like species in chaetothyriales with ant-associated life styles

Quan Y, Ahmed SA, Menezes da Silva N, Al-Hatmi AMS, Mayer VE, Deng S, et al.

Fungal Biol, 2021 04;125(4):276-284.
PMID: 33766306 DOI: 10.1016/j.funbio.2020.11.006

Among ancestral fungi in Chaetothyriales, several groups have a life style in association with tropical ants, either in domatia or in carton-nests. In the present study, two strains collected from ant carton in Thailand and Malaysia were found to represent hitherto undescribed species. Morphological, physiological, phylogenetic data and basic genome information are provided for their classification. Because of the relatively large phylogenetic distances with known species confirmed by overall genome data, large subunit (LSU) and Internal Transcribed Spacer (ITS) ribosomal DNA sequences were sufficient for taxonomic circumscription of the species. The analyzed strains clustered with high statistical support as a clade in the family Trichomeriaceae. Morphologically they were rather similar, lacking sporulation in vitro. In conclusion, Incumbomyces delicatus and Incumbomyces lentus were described as new species based on morphological, physiological and phylogenetic analysis.
Fulltext Graphene-based hybrid nanoparticle of doxorubicin for cancer chemotherapy

SreeHarsha N, Maheshwari R, Al-Dhubiab BE, Tekade M, Sharma MC, Venugopala KN, et al.

Int J Nanomedicine, 2019;14:7419-7429.
PMID: 31686814 DOI: 10.2147/IJN.S211224

Background: Prostate cancer (PC) has the highest prevalence in men and accounts for a high rate of neoplasia-related death. Doxorubicin (DOX) is one of the most widely used anti-neoplastic drugs for prostate cancer among others. However, it has low specificity and many side effects and affects normal cells. More recently, there have been newly developed drug delivery tools which are graphene or graphene-based, used to increase the specificity of the delivered drug molecules. The graphene derivatives possess both π-π stacking and increased hydrophobicity, factors that increase the likelihood of drug delivery. Despite this, the hydrophilicity of graphene remains problematic, as it induced problems with stability. For this reason, the use of a chitosan coating remains one way to modify the surface features of graphene.
Method: In this investigation, a hybrid nanoparticle that consisted of a DOX-loaded reduced graphene oxide that is stabilized with chitosan (rGOD-HNP) was developed.
Result: The newly developed rGOD-HNP demonstrated high biocompatibility and efficiency in entrapping DOX (~65%) and releasing it in a controlled manner (~50% release in 48 h). Furthermore, it was also demonstrated that rGOD-HNP can intracellularly deliver DOX and more specifically in PC-3 prostate cancer cells.
Conclusion: This delivery tool offers a feasible and viable method to deliver DOX photo-thermally in the treatment of prostate cancer.
Synthesis, X-ray crystal and monoamine oxidase inhibitory activity of 4,6-dihydrobenzo[c]pyrano[2,3-e][1,2]thiazine 5,5-dioxides: In vitro studies and docking analysis

Ahmad S, Jalil S, Zaib S, Aslam S, Ahmad M, Rasul A, et al.

Eur J Pharm Sci, 2019 Apr 01;131:9-22.
PMID: 30735822 DOI: 10.1016/j.ejps.2019.02.007

We report the synthesis and biological evaluation of two new series of 2-amino-6-benzyl-4-phenyl-4,6-dihydrobenzo[c]pyrano[2,3-e][1,2]thiazine-3‑carbonitrile 5,5-dioxides and 2-amino-6-methyl-4-phenyl-4,6-dihydrobenzo[c]pyrano[2,3-e][1,2]thiazine-3‑carbonitrile 5,5-dioxides. The synthetic methodology involves a multistep reaction starting with methyl anthranilate which was coupled with methane sulfonyl chloride. The product of the reaction was subjected to N-benzylation and N-methylation reactions followed by ring closure with sodium hydride resulting in the formation of respective 2,1-benzothiazine 2,2-dioxides. These 2,1-benzothiazine precursors were subjected to multicomponent reaction with malononitrile and substituted benzaldehydes for the synthesis of two new series of pyranobenzothiazines (6a-r and 7a-r). The synthesized compounds were screened as selective inhibitors of monoamine oxidase A and monoamine oxidase B. The in vitro results suggested that compound 6d and 7q are the selective inhibitors of monoamine oxidase A, however, the selective and potent inhibitors of monoamine oxidase B included compounds 6h and 7r. Moreover, some dual inhibitors were noticed like 7l having more inhibitory activity towards both the isozymes. Moreover, the binding modes of the selective and potent inhibitors of monoamine oxidase A and B were investigated by molecular docking analysis. The results suggested that the synthetic derivatives may be potential towards the monoamine oxidase isozymes.
Fulltext Aggregation behavior of cetyldimethylethylammonium bromide under the influence of bovine serum albumin in aqueous/electrolyte solutions at various temperatures and compositions: conductivity and molecular dynamics study

Ahmed MF, Molla MR, Saha M, Shahriar I, Rahman MS, Halim MA, et al.

RSC Adv, 2019 Feb 22;9(12):6556-6567.
PMID: 35518479 DOI: 10.1039/c9ra00070d

Herein, we have investigated the interaction of bovine serum albumin (BSA), the most abundant globular protein, with a conventional cationic surfactant, cetyldimethylethylammonium bromide (CDMEAB), through a conductivity technique in the absence/presence of electrolyte solutions at various temperatures (298.15-323.15 K). The interaction of the protein with drugs/surfactants and other additives plays a crucial role in the body. Hence, the main concern of the study is to extract the impact of BSA on surfactant molecules and vice versa. From the specific conductivity versus concentration of surfactant plots, three different noticeable critical micelle concentration (c*) values were obtained for pure CDMEAB and its mixture with protein/protein + salts. The presence of BSA and electrolytes altered the c* values of CDMEAB revealing interactions among the studied constituents where the salt solutions reduced the c* values and created a convenient environment for favorable micellization. The negative magnitudes achieved for standard free energy changes (ΔG 0 m) suggest spontaneity of micellization while the values of ΔH 0 m and ΔS 0 m signified the existence of some electrostatic and hydrophobic interactions. The values of molar heat capacity (ΔC 0 m) were positive as well as small which was an indication of less structural deformation. Molecular Dynamics (MD) simulation for all atoms revealed that the salt ions promoted non-covalent interaction between BSA and CDMEAB, and such interactions were not observed in the absence of the salt. Protein structure remained nearly same in spite of strong interaction with CDMEAB as evident from the overall RMSD (root-mean-square deviation) values of the alpha carbons and backbone of the protein and RMSF (root-mean-square fluctuation) values of the amino acid residues present in BSA. In this work thermodynamic parameters of transfer (such as ΔG 0 m.tr., ΔH 0 m.tr., and ΔC 0 p.m.tr.) were also evaluated and the results are discussed in detail. Besides, contributions of enthalpy and entropy to free energy changes were also analyzed.

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